ArticleEuropean journal of nuclear medicine and molecular imaging2008
Development and evaluation of peptidic ligands targeting tumour-associated urokinase plasminogen activator receptor (uPAR) for use in alpha-emitter therapy for disseminated ovarian cancer.
Article in European journal of nuclear medicine and molecular imaging, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 47 citations in OpenAlex.
- Review
- Towards the Magic Radioactive Bullet: Improving Targeted Radionuclide Therapy by Reducing the Renal Retention of Radioligands.Pharmaceuticals (Basel, Switzerland) · 2024Review
- The Urokinase Receptor (uPAR) as a "Trojan Horse" in Targeted Cancer Therapy: Challenges and Opportunities.Cancers · 2021Review
- Targeting the Urokinase-Type Plasminogen Activator Receptor (uPAR) in Human Diseases With a View to Non-invasive Imaging and Therapeutic Intervention.Frontiers in cell and developmental biology · 2021Review
- Development of Targeted Alpha Particle Therapy for Solid Tumors.Molecules (Basel, Switzerland) · 2019Review
- Multifaceted Role of the Urokinase-Type Plasminogen Activator (uPA) and Its Receptor (uPAR): Diagnostic, Prognostic, and Therapeutic Applications.Frontiers in oncology · 2018Review
- Be Active or Not: the Relative Contribution of Active and Passive Tumor Targeting of Nanomaterials.Nanotheranostics · 2017Review
- Isothiocyanate-Functionalized Bifunctional Chelates and fac-[M(I)(CO)3](+) (M = Re, (99m)Tc) Complexes for Targeting uPAR in Prostate Cancer.Bioconjugate chemistry · 2016Article
- Imaging of human pancreatic cancer xenografts by single-photon emission computed tomography withOncology letters · 2015Article
- Toward a magic or imaginary bullet? Ligands for drug targeting to cancer cells: principles, hopes, and challenges.International journal of nanomedicine · 2015Review
- A novel tumor targeting drug carrier for optical imaging and therapy.Theranostics · 2014Article
- Improved PET imaging of uPAR expression using new (64)Cu-labeled cross-bridged peptide ligands: comparative in vitro and in vivo studies.Theranostics · 2013Article
- Structure-driven design of radionuclide tracers for non-invasive imaging of uPAR and targeted radiotherapy. The tale of a synthetic peptide antagonist.Theranostics · 2013Review
- The many spaces of uPAR: delivery of theranostic agents and nanobins to multiple tumor compartments through a single target.Theranostics · 2013Review
- Urokinase plasminogen activator receptor (uPAR) targeted nuclear imaging and radionuclide therapy.Theranostics · 2013Review
- Near-infrared fluorescent divalent RGD ligand for integrin αvβ₃-targeted optical imaging.Bioorganic & medicinal chemistry letters · 2012Article
- Therapeutic efficacy and toxicity of 225Ac-labelled vs. 213Bi-labelled tumour-homing peptides in a preclinical mouse model of peritoneal carcinomatosis.European journal of nuclear medicine and molecular imaging · 2012Article
- Stroma targeting nuclear imaging and radiopharmaceuticals.International journal of molecular imaging · 2012Article
- Targeting the urokinase plasminogen activator receptor inhibits ovarian cancer metastasis.Clinical cancer research : an official journal of the American Association for Cancer Research · 2011Article
- Development of novel therapeutics targeting the urokinase plasminogen activator receptor (uPAR) and their translation toward the clinic.Current pharmaceutical design · 2011Article
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeAmong gynecologic malignancies, ovarian cancer has the highest mortality due to rapid peritoneal dissemination. Treatment failure particularly arises from failure to eliminate disseminated cells. Our aim was to develop peptidic radioligands targeting tumour cell-associated urokinase receptor (uPAR, CD87) for alpha-emitter therapy for advanced ovarian cancer.
methodsDOTA-conjugated, uPAR-directed ligands were synthesised on solid-phase. Binding of peptides to human cells expressing uPAR was assayed by flow cytofluorometry or, in case of (213)Bi-labelled peptides, by measuring cell-bound radioactivity. Bio-distribution of the (213)Bi-labelled peptide P-P4D was analysed in nude mice 28 days after intraperitoneal inoculation of OV-MZ-6 ovarian cancer cells in the absence or presence of the plasma expander gelofusine.
resultsuPAR-selective ligands were developed based on published high-affinity uPAR-binding peptides. For preparation of N-terminally cross-linked divalent ligands, a novel solid-phase procedure was developed. Specific binding of (213)Bi-labelled peptides to monocytoid U937 and OV-MZ-6 cells was demonstrated using the natural ligand of uPAR, pro-uPA, or a soluble form of uPAR, suPAR, as competitors. The pseudo-symmetrical covalent dimer (213)Bi-P-P4D displayed superior binding to OV-MZ-6 cells in vitro. Accumulation of (213)Bi-P-P4D in tumour tissue was demonstrated by bio-distribution analysis in nude mice bearing intraperitoneal OV-MZ-6-derived tumours. Gelofusine reduced kidney uptake of (213)Bi-P-P4D by half.
conclusionOvarian cancer cells overexpressing uPAR were specifically targeted in vitro and in vivo by (213)Bi-P-P4D. Kidney uptake of (213)Bi-P-P4D was distinctly reduced using gelofusine. Thus, this radiopeptide may represent a promising option for therapy for disseminated ovarian cancer.
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